CAS: 132834-58-3; 1-(5-(Trifluoromethyl)Pyridin-2-yl)Piperazine

该化合物是一种化学化合物,其独特结构包括一个管子环和一种以三氟甲基组替代的,其特性包括一个三氟甲基组;该三氟甲基组的存在会增强该化合物的亲脂性,并可能影响其生物活动,使其对药用化学感兴趣;该化合物通常具有中度至高溶解有机溶剂等特性,而其溶解于水中的溶解性可能因具体情况而不同;该管子环具有制药业的潜力,经常与各种生物活动有关,包括...

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87394-63-6 120298-11-5 128263-65-0

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2-chloro-5-trifluoromethylpyridine piperazine 2-bromo-5-(trifluoromethyl)pyridine 2-methyl-2-[4-(5-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-propionic acid 4-[4-(5-Trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-benzoic acid tert-butyl ester (2R)-2-{4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}propanoic acid

合成工艺路线路线简述

    📜2-溴-5-(三氟甲基)吡啶置于tris-(Dibenzylideneacetone)Dipalladium(0),R-(+)-1,1'-联萘-2,2'-双二苯膦,三氟乙酸,Sodium T-Butanolate体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 15.0H,反应生成1-[5-(三氟甲基)-2-吡啶基]哌嗪
    参考文献:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
    标题:具有混合结构的新型苯甘氨酰胺衍生物可作为新型广谱抗惊厥药的候选者
    摘要:在本研究中,应用集中的组合化学方法将众所周知的 Trpv1 拮抗剂的结构片段与我们小组先前发现的强效抗惊厥先导化合物ka-104合并.因此,在体内和体外试验中设计,合成和表征了一系列 22 种原始化合物.获得的化合物在最大电击 (Mes) 测试和 6 Hz 癫痫模型(使用 32 和 44 Ma 电流强度)中显示出强大的体内抗癫痫活性.最有效的化合物53和60显示出以下药理学特征:Ed 50 = 89.7 Mg/kg (Mes),Ed 50 = 29.9 Mg/kg (6 Hz,32 Ma),Ed 50= 68.0 Mg/kg (6 Hz,44 Ma),Ed 50 = 73.6 Mg/kg (Mes),Ed 50 = 24.6 Mg/kg (6 Hz,32 Ma),Ed 50 = 56.3 Mg/kg (6赫兹,44毫安),分别.此外,53和60对iv Ptz 癫痫发作阈值有效,
    Doi:10.3390/cells11121862

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    专利信息


    专利号:US-2015239796-A1
    优先权日:2014-02-19
    标题:One pot synthesis of 18f labeledtrifluoromethylated compounds with difluoro(iodo)methane
    发明人:RüHL THOMAS; RISS PATRICK; RAFIQUE WAQAS
    权利人:UNIV OSLO
    摘要:The present invention relates to compositions and methods for the synthesis of 18 F labeled compounds. In particular, the present invention relates to a copper (I) mediated one pot method for 18 F-trifluoromethylation of aromatic- or heteroaromatic halides with difluoro(iodo)methane (e.g., for use at PET imaging agents).

    专利号:US-10995078-B2
    优先权日:2013-03-13
    标 题:Compounds and compositions for inhibition of FASN
    发明人:BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
    权利人:FORMA THERAPEUTICS INC
    摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

    专利号:US-9676721-B2
    优先权日:2010-09-03
    标题 :Compounds and compositions for the inhibition of NAMPT
    发明人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
    权利人:BAIR KENNETH W; BUCKMELTER ALEXANDRE J; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
    摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.

    专利号:US-9555039-B2
    优先权日:2011-05-09
    标题:Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT)
    发明人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
    权利人:BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; KUNTZ JUDITH D; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
    摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below: Formula (I)

    专利号:US-9169209-B2
    优先权日:2011-05-04
    标题:Compounds and compositions for the inhibition of NAMPT
    发明人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG
    权利人:BAIR KENNETH W; BAUMEISTER TIMM; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; FORMA TM LLC
    摘要:The present invention relates to compounds and composition for inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below.

    专利号:US-8318928-B2
    优先权日:2008-12-15
    标题 :Fused imidazole carboxamides as TRPV3 modulators
    发明人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
    权利人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI; GLENMARK PHARMACEUTICALS SA
    摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.

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    合成参考文献


    参考文献:10.1055/s-0030-1257906
    摘要:Dömling A, Huang Y. Piperazine Scaffolds via Isocyanide-Based Multicomponent Reactions. Synthesis. 2010 Jul 30;2010(17):2859–83. doi: 10.1055/s-0030-1257906.
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